公开(公告)号：US20110281881A1

公开(公告)日：2011-11-17

申请号：US13144554

申请日：2010-02-02

申请人： Henricus, Jacobus, Maria Gijsen ,  Adriana Ingrid Velter ,  Gregor James MacDonald ,  Francois Paul Bischoff ,  Tongfei Wu ,  Sven, Franciscus, Anna Van Brandt ,  Michel Surkyn ,  Mirko Zaja ,  Serge, Maria, Aloysius Pieters ,  Didier Jean-Claude Berthelot ,  Michel, Anna, Josef De Cleyn ,  Daniel Oehlrich

发明人： Henricus, Jacobus, Maria Gijsen ,  Adriana Ingrid Velter ,  Gregor James MacDonald ,  Francois Paul Bischoff ,  Tongfei Wu ,  Sven, Franciscus, Anna Van Brandt ,  Michel Surkyn ,  Mirko Zaja ,  Serge, Maria, Aloysius Pieters ,  Didier Jean-Claude Berthelot ,  Michel, Anna, Josef De Cleyn ,  Daniel Oehlrich

IPC分类号： A61K31/437 ,  C07D403/12 ,  C07D413/14 ,  C07D403/14 ,  C07D487/04 ,  C07D413/12 ,  C07D417/12 ,  C07D401/14 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/5025 ,  A61K31/4985 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/444 ,  A61K31/501 ,  A61P25/28 ,  A61P25/00 ,  A61P25/16 ,  C07D471/04

CPC分类号： C07D487/04 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

摘要： The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及其中Het1，Het2，A1，A2，A3和A4具有权利要求中限定的含义的式（I）的取代双环杂环化合物。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US08987276B2

公开(公告)日：2015-03-24

申请号：US14005598

申请日：2012-03-22

申请人： Francois Paul Bischoff ,  Adriana Ingrid Velter ,  Sven Franciscus Anna Van Brandt ,  Didier Jean-Claude Berthelot

发明人： Francois Paul Bischoff ,  Adriana Ingrid Velter ,  Sven Franciscus Anna Van Brandt ,  Didier Jean-Claude Berthelot

IPC分类号： A61K31/496 ,  A61K31/506 ,  C07D249/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D249/10

CPC分类号： C07D403/04 ,  C07D249/10 ,  C07D401/14

摘要： The present invention is concerned with novel substituted triazolyl piperazine and triazolyl piperidine derivatives of Formula (I) wherein R1, R2, R3, R4a, R4b, R5, X, Y1, Y2, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新型取代的三唑基哌嗪和三唑基哌啶衍生物，其中R1，R2，R3，R4a，R4b，R5，X，Y1，Y2，L1和L2具有权利要求中限定的含义。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US08946426B2

公开(公告)日：2015-02-03

申请号：US13144554

申请日：2010-02-02

申请人： Henricus Jacobus Maria Gijsen ,  Adriana Ingrid Velter ,  Gregor James MacDonald ,  François Paul Bischoff ,  Tongfei Wu ,  Sven Franciscus Anna Van Brandt ,  Michel Surkyn ,  Mirko Zaja ,  Serge Maria Aloysius Pieters ,  Didier Jean-Claude Berthelot ,  Michel Anna Jozef De Cleyn ,  Daniel Oehlrich

发明人： Henricus Jacobus Maria Gijsen ,  Adriana Ingrid Velter ,  Gregor James MacDonald ,  François Paul Bischoff ,  Tongfei Wu ,  Sven Franciscus Anna Van Brandt ,  Michel Surkyn ,  Mirko Zaja ,  Serge Maria Aloysius Pieters ,  Didier Jean-Claude Berthelot ,  Michel Anna Jozef De Cleyn ,  Daniel Oehlrich

IPC分类号： A61K31/437 ,  C07D471/04 ,  C07D487/04 ,  C07D403/10 ,  C07D413/10

CPC分类号： C07D487/04 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

摘要： The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及其中Het1，Het2，A1，A2，A3和A4具有权利要求中限定的含义的式（I）的取代双环杂环化合物。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US20140011816A1

公开(公告)日：2014-01-09

申请号：US14005598

申请日：2012-03-22

申请人： Francois Paul Biscoff ,  Adriana Ingrid Velter ,  Sven Franciscus Anna Van Brandt ,  Didier Jean-Claude Berthelot

发明人： Francois Paul Biscoff ,  Adriana Ingrid Velter ,  Sven Franciscus Anna Van Brandt ,  Didier Jean-Claude Berthelot

IPC分类号： C07D403/04 ,  C07D401/14

CPC分类号： C07D403/04 ,  C07D249/10 ,  C07D401/14

摘要： The present invention is concerned with novel substituted triazolyl piperazine and triazolyl piperidine derivatives of Formula (I) wherein R1, R2, R3, R4a, R4b, R5, X, Y1, Y2, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新型取代的三唑基哌嗪和三唑基哌啶衍生物，其中R1，R2，R3，R4a，R4b，R5，X，Y1，Y2，L1和L2具有权利要求中限定的含义。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US09115143B2

公开(公告)日：2015-08-25

申请号：US14233078

申请日：2012-07-12

申请人： Garrett Berlond Minne ,  François Paul Bischoff ,  Henricus Jacobus Maria Gijsen ,  Adriana Ingrid Velter ,  Serge Maria Aloysius Pieters ,  Didier Jean-Claude Berthelot

发明人： Garrett Berlond Minne ,  François Paul Bischoff ,  Henricus Jacobus Maria Gijsen ,  Adriana Ingrid Velter ,  Serge Maria Aloysius Pieters ,  Didier Jean-Claude Berthelot

IPC分类号： C07D498/04 ,  C07D487/04

CPC分类号： C07D498/04 ,  C07D487/04

摘要： The present invention is concerned with novel substituted indole derivatives of Formula (I) wherein R1, R2, R3, A1, A2, A3, Y and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新型取代吲哚衍生物，其中R1，R2，R3，A1，A2，A3，Y和X具有权利要求中限定的含义。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：US20140148450A1

公开(公告)日：2014-05-29

申请号：US14233078

申请日：2012-07-12

申请人： Garrett Berlond Minne ,  François Paul Bischoff ,  Henricus Jacobus Maria Gijsen ,  Adriana Ingrid Velter ,  Serge Maria Aloysius Pieters ,  Didier Jean-Claude Berthelot

发明人： Garrett Berlond Minne ,  François Paul Bischoff ,  Henricus Jacobus Maria Gijsen ,  Adriana Ingrid Velter ,  Serge Maria Aloysius Pieters ,  Didier Jean-Claude Berthelot

IPC分类号： C07D498/04

CPC分类号： C07D498/04 ,  C07D487/04

摘要： The present invention is concerned with novel substituted indole derivatives of Formula (I) wherein R1, R2, R3, A1, A2, A3, Y and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

摘要翻译： 本发明涉及式（I）的新型取代吲哚衍生物，其中R1，R2，R3，A1，A2，A3，Y和X具有权利要求中限定的含义。 根据本发明的化合物可用作γ-分泌酶调节剂。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。